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Molecules 2017, 22(3), 369; doi:10.3390/molecules22030369

Antiprotozoal Activity of Triazole Derivatives of Dehydroabietic Acid and Oleanolic Acid

1
Laboratorio de Química de Productos Naturales, Instituto de Química de Recursos Naturales, Universidad de Talca, 3460000 Talca, Chile
2
Centro para el Desarrollo de la Investigación Científica (CEDIC), Manduvirá 635 entre 15 de Agosto y O’Leary, Barrio La Encarnación 1255, 2511 Asunción, Paraguay
*
Author to whom correspondence should be addressed.
Academic Editor: Jean-Marc Sabatier
Received: 23 January 2017 / Revised: 13 February 2017 / Accepted: 21 February 2017 / Published: 28 February 2017
(This article belongs to the Special Issue Structure-Activity Relationship of Natural Products)
View Full-Text   |   Download PDF [412 KB, uploaded 28 February 2017]   |  

Abstract

Tropical parasitic diseases such as Chagas disease and leishmaniasis are considered a major public health problem affecting hundreds of millions of people worldwide. As the drugs currently used to treat these diseases have several disadvantages and side effects, there is an urgent need for new drugs with better selectivity and less toxicity. Structural modifications of naturally occurring and synthetic compounds using click chemistry have enabled access to derivatives with promising antiparasitic activity. The antiprotozoal activity of the terpenes dehydroabietic acid, dehydroabietinol, oleanolic acid, and 34 synthetic derivatives were evaluated against epimastigote forms of Trypanosoma cruzi and promastigotes of Leishmaniabraziliensis and Leishmania infantum. The cytotoxicity of the compounds was assessed on NCTC-Clone 929 cells. The activity of the compounds was moderate and the antiparasitic effect was associated with the linker length between the diterpene and the triazole in dehydroabietinol derivatives. For the oleanolic acid derivatives, a free carboxylic acid function led to better antiparasitic activity. View Full-Text
Keywords: cytotoxicity; dehydroabietic acid; Leishmania spp.; oleanolic acid; triazole derivatives; Trypanosoma cruzi cytotoxicity; dehydroabietic acid; Leishmania spp.; oleanolic acid; triazole derivatives; Trypanosoma cruzi
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Pertino, M.W.; Vega, C.; Rolón, M.; Coronel, C.; Rojas de Arias, A.; Schmeda-Hirschmann, G. Antiprotozoal Activity of Triazole Derivatives of Dehydroabietic Acid and Oleanolic Acid. Molecules 2017, 22, 369.

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